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试论用17荧光雌酮测定雌激素受体和生化法的关系

BINDING MECHANISM OF 17-FLUORI-ESTRONE WITH ESTROGEN RECEPTOR IN HISTOCHEMICAL AND BIOCHEMICAL ASSAYS

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【作者】 张慧影励舜华

【Author】 Zhang,Hui-ying Li,Shun-hua(Laboratory of Biochemistry,Beijing Institute for Cancer Research,Beijing)

【机构】 北京市肿瘤防治研究所生化室北京市肿瘤防治研究所生化室 北京北京

【摘要】 本文对采用细胞化学法测定乳腺癌内雌激素受体[ER]所用的荧光配体17-FE是否也是与ER上结合位点相结合的问题进行了探讨。在测定17-FE对[3H]E2与兔子宫上清液内ER结合的影响后,指出:17-FE对[3H]E2与ER的结合具有抑制作用,且其抑制作用随着17-FE浓度的提高而加大。在一系列不同浓度[3H]E2下测定其与ER的特异结合,同时测定加入不同浓度17-FE后的特异结合量,以Lineweaver-Burk和Scate-bard法分别作图。分析结果均显示为竞争性抑制曲线,可见17-FE和[3H]E2一样是与兔子宫上清液内ER上的结合位点相结合的。因此采用细胞化学法测定ER时,17-FE是一理想的配体。

【Abstract】 Fluorescein labeled estrone at the 17th carbon (17-FE) was used as a ligand for cytochemical evaluation of the estrogen receptor (ER) in human breast cancer.Possibility of 17-FE and (3H)E2 binding to the same ER sites was investigated.Addition of various concentrations of 17-FE in (3H)E2 binding system showed that 17-FE could inhibit the (3H)E2 specific binding.Specific binding of (3H)E2 at different concentrations in the presence of various concentrations of 17-FE was measured.Lineweaver-Burk and Scatchard plot were used for analysis.From these curves competition of 17-FE with (3H)E2 for a common binding site was suggested,and 17FE seemed to be an ideal ligand for cytochemical determination of ER in human breast cancer.

【关键词】 雌激素受体17-FE竞争性抑制作用
【Key words】 Estrogen receptor17-FEcompetitive inhibition
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